LQZ-7I is an Orally Active Survivin-Targeting Inhibitor

Survivin is a member of the inhibitor of apoptosis (IAP) protein family that inhibits caspases and blocks cell death. Caspases highly expressed in most cancers and are associate with a poor clinical outcome. The differential expression of survivin in cancer cells compared to normal tissues and its role as...

Targapremir-210, a Selective miR-210 Inhibitor, Targets the Dicer Site in Pre-miR-210

Hypoxia is a non-physiological level of oxygen tension, a phenomenon common in a majority of malignant tumors. Hypoxia associates with tumor progression, resistance to therapy, and metastasis in cancer. Numerous pathways play critical roles in cancer maintenance, including noncoding RNAs such as microRNA (miR)-210 that regulates hypoxia-inducible factors. In...

GSK621 is a Specific AMPK Activator, Inducing Autophagy and Apoptosis

AMPK is an enzyme, which plays a role in cell energy homeostasis. It mainly activates glucose and fatty acid uptake and oxidation when the cell energy is low. Specifically, AMPK is a major regulator of cell metabolism, which can exert its carcinogenic or antitumor activities. Besides, the activation of...

HLI373 is an Efficacious Hdm2 Inhibitor, with Antimalarial Activity

Hdm2 is an ubiquitin-protein ligase. Hdm2 suppresses the transcriptional activity of the tumor suppressor p53 and promotes its degradation. HLI373 is an efficacious Hdm2 inhibitor. HLI373 is effective in inducing apoptosis of several tumor cell lines that are sensitive to DNA-damaging agents. These results suggest that HLI373 could serve...

XMU-MP-3 is a Potent Non-Covalent BTK Inhibitor and Induces Apoptosis

BTK, a nonreceptor tyrosine kinase member of the Tec kinase family, plays a significant role in B-cell development. BTK is a unique therapeutic target in B-cell malignancies. XMU-MP-3, a noncovalent inhibitor with potent BTK inhibitory. XMU-MP-3 suppresses BTK kinase activity both in vitro and in vivo. In addition, XMU-MP-3...

DI-87 is an Orally Active and Selective Deoxycytidine Kinase (dCK) Inhibitor

Deoxyribonucleotide triphosphates (dNTPs) are essential for tumor growth, and DNA replication and repair also is essential dNTPs.  Parallel and convergent de novo and salvage pathways redundantly produce the same dNTPs using different substrates.  The de novo pathway produces dNTPs from glucose and amino acids and is dependent upon ribonucleotide reductase (RNR)....